TEAD–YAP Interaction Inhibitors and MDM2 Binders from DNA-Encoded Indole-Focused Ugi Peptidomimetics

DNA-encoded combinatorial synthesis provides efficient and dense coverage of chemical space around privileged molecular structures. The indole side chain of tryptophan plays a prominent role in key, or “hot spot”, regions of protein–protein interactions. A DNA-encoded combinatorial peptoid library was designed based on the Ugi four-component reaction by employing tryptophan-mimetic indole side chains to probe the surface of target proteins. Several peptoids were synthesized on a chemically stable hexathymidine adapter oligonucleotide “hexT”, encoded by DNA sequences, and substituted by azide-alkyne cycloaddition to yield a library of 8112 molecules. Selection experiments for the tumor-relevant proteins MDM2 and TEAD4 yielded MDM2 binders and a novel class of TEAD-YAP interaction inhibitors that perturbed the expression of a gene under the control of these Hippo pathway effectors.     

Correction to: Tissue free water tritium (TFWT) and organically bound tritium (OBT) in marine eco system at Tarapur on the west coast of India

Journal of Radioanalytical and Nuclear Chemistry - The original publication of the article contains errors in the text and Tables 3, 4 and 5. The corrected text and tables are provided in...     

Fluence Rate Determines PDT Efficiency in Breast Cancer Cells Displaying Different GSH Levels

Photodynamic therapy (PDT) appears as a promising alternative in the treatment of breast cancer since it can be highly effective in curing cancer while preserving normal tissue. However, predicting outcomes in PDT still constitutes a great challenge. One of the parameters that are usually empirically determined is the rate of photon flux delivered to the tissue (light fluence rate). In the present study, we intended to understand why monolayers of human cells derived from mammary adenocarcinomas (MDA-MB-231 and MCF-7) respond quite differently to fluence rates (cells were irradiated either for 6 or for 16 min) at a fixed light dose (4.5 J cm⁻²) delivered with an array of LEDs in a typical methylene blue PDT protocol. While death rates of MDA-MB-231 cells were insensitive to the fluence rate, MCF-7 cells showed a quite impressive (three times) decrease in cell death levels in the shorter irradiation protocol. Independent on cell type cell death was invariably correlated with the depletion of reduced glutathione intracellular levels and consequently with widespread redox misbalance. Our data show the potential to optimize fluence rates to provide exhaustion of the cell antioxidant responses in order to circumvent therapy resistance of breast tumors.     

Sustainable preparation of gold nanoparticles via green chemistry approach for biogenic applications

Novel premises of ‘Green Nanotechnology’ have tremendous impacts towards industrial scale revolution. The furtive extracted from natural precursors have driven to the generation of biogenic resources for the fabrication of cutting-edge nanomaterials in simple and cost-effective process. This inspection is an intension of the coupling hypothesis of Nanotechnology via ‘Green-Chemistry’ avenue. So, as to diminish the negative effects of technological applications in the health of human beings and the environment, society is focused towards a greener future. Nanoscience assures a promising future by its improvement in green chemistry to develop the 'Greenary Nanoscience and Nanotechnology'. The improvement and execution of chemical assisted processes in order to reduce the usage of harmful substances, the ‘Green Chemistry’ approach is one and only remarkable authentication, which attributed to long range surface area and higher pore volume of gold-nanoparticles. As of now, the efficient biogenic mechanism dramatically reduces the utilization and hazardous reagents have been employed to low-price natural and waste products to yield value-added nanomaterials with extensive relevance, suggesting an economical and green solution to environmental issues. In depth investigation of this critical review illustrates, novel biogenic screening platform was also conducted against antimicrobial strains and degradation of gold-nanoparticles products well explored-from selection precursors evolved from natural extracts, as well as eventually disintegration into bio-degradable yet potentially recyclable byproducts.     

Sodium sulfate influence on the electrodeposition of MnO2 films for application in Supercapacitors

Journal of Solid State Electrochemistry - Manganese dioxide (MD) was synthesized by cyclic voltammetry using 0.5 mol L−1 MnSO4·6H2O as the precursor solution, with and...     

Tailoring a Zinc Oxide Nanorod Surface by Adding an Earth-Abundant Cocatalyst for Induced Sunlight Water Oxidation

Herein, a detailed investigation of the surface modification of a zinc oxide (ZnO) nanorod electrode with FeOOH nanoparticles dispersed in glycine was conducted to improve the water oxidation reaction assisted by sunlight. The results were systematically analysed in terms of the general parameters (light absorption, charge separation, and surface for catalysis) that govern the photocurrent density response of metal oxide as photoanode in a photoelectrochemical (PEC) cell. ZnO electrodes surface were modified with different concentration of FeOOH nanoparticles using the spin-coating deposition method, and it was found that 6-layer deposition of glycine-FeOOH nanoparticles is the optimum condition. The glycine plays an important role decreasing the agglomeration of FeOOH nanoparticles over the ZnO electrode surface and increasing the overall performance. Comparing bare ZnO electrodes with the ones modified with glycine-FeOOH nanoparticles an enhanced photocurrent density can be observed from 0.27 to 0.57 mA/cm² at 1.23 V_RHE under sunlight irradiation. The impedance spectroscopy data aid us to conclude that the higher photocurrent density is an effect associated with more efficient surface for chemical reaction instead of electronic improvement. Nevertheless, the charge separation efficiency remains low for this system. The present discovery shows that the combination of glycine-FeOOH nanoparticle is suitable and environmentally-friend cocatalyst to enhance the ZnO nanorod electrode activity for the oxygen evolution reaction assisted by sunlight irradiation.     

Determination of phenolic compounds,in vitro antioxidant activity and characterization of secondary metabolites in different parts of Passiflora cincinnata by HPLC-DAD-MS/MS analysis

Abstract

Ethanol extracts of different parts of Passiflora cincinnata were obtained by maceration. The total phenolic and flavonoid contents were evaluated. The antioxidant activities were determined by β-carotene-linoleic acid bleaching test, 2,2-diphenyl-1-picrylhydrazil (DPPH), and 2,2’-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging. The crude ethanol stem extract showed the highest amount of total polyphenols (45.53?mg gallic acid equivalent/g) while the highest total flavonoid contents (1.42?mg of quercetin equivalent/g) were observed in the leaf extract. The lowest IC₅₀ (25.65?μg/ml) by the DPPH method was observed for the stem extract. The ABTS method showed a significant antioxidant activity for all investigated extracts. The secondary metabolite composition of ethanol extracts was assessed by HPLC-DAD-MS/MS analysis, leading to the identification of fourteen secondary metabolites in P. cincinnata extracts. These results showed the potentiality of this species as a source of phenolic compounds and antioxidants.     

Cationic ≠3-allylmetal complexes, 13a) electrical properties of new poly(phenylacetylene) obtained from nickel catalysts

Monometallic complexes of Nickel have been successfully, tested in reaction with olefinic and acetylenic compounds. This paper is devoted to one of the resulting products, a polyphenylacetylene which presents interesting properties. It is readily obtained avoiding the step of a polymer precursor; it is soluble in several solvents, stable in air up to 200° C and may possess a rather high conductivity, depending on polymerization conditions. This is a noticeable difference versus previously reported polyphenylacetylenes which were insulating materials.     

Transient dynamic analysis of cracked structures with multiple contact pairs using generalized HSNC

Nonlinear Dynamics - The development of efficient computational methods for cracked structures is critical in the fields of civil, mechanical, and aerospace engineering since the influence of...